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Activated charcoal surface area and its role in multiple-dose charcoal therapy.

The study hypothesis was to prove that increasing the surface area (SA) of activated charcoal (AC) will enhance theophylline elimination in multiple-dose AC therapy. Five healthy, nonsmoking, nonmedicated, volunteer men ranging from the ages of 18 to 24 years old were entered onto the study. A prospective, randomized, crossover study was conducted with each subject serving as their own control. Subjects fasted overnight before receiving 8 mg/kg of intravenous theophylline at the beginning of a control phase and two study phases. No AC was administered in the control phase. Two experimental phases compared Actidose Aqua AC (1,500 m2/g; Paddock Laboratories, Inc, Minneapolis, MN) with Norit A Supra AC (2,000 m2/g; Norit NV, Amersfoort, the Netherlands). In each phase, 50 g of the AC was administered orally after the conclusion of the theophylline infusion. Subsequent 50-g doses of the AC preparation were administered at 4 and 8 hours after the initial dose of AC. Serial blood samples for theophylline level determinations were obtained at 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 10.0, and 12.0 hours after the completion of the theophylline infusion. For each of the three data sets, the absolute area under the absorption curve (A-AUC) was calculated to infinity using the trapezoidal rule. Additionally, the relative area under the absorption curve (R-AUC) was determined for each data set. Data were analyzed using repeated measures of analysis of variance (ANOVA) and Tukey's test. The alpha error was set at 0.05.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Oral↗

Pediatric ingestions: charcoal alone versus ipecac and charcoal.

STUDY OBJECTIVES: To determine the effect of syrup of ipecac (SOI) on time to receive and retention of activated charcoal (AC) and on total ED time. DESIGN: During a two-year period, patients were enrolled in a prospective, randomized, unblinded, controlled trial. SETTING: All patients were recruited and studied in a pediatric emergency department. PARTICIPANTS: Seventy children less than 6 years old (mean age, 2.4 +/- 0.2 years) who presented with mild-to-moderate acute oral ingestions. INTERVENTIONS: Group 1 received SOI before AC. Group 2 received only AC. MEASUREMENTS AND MAIN RESULTS: Group 1 patients took significantly longer to receive AC than group 2 from the time of ED arrival (2.6 +/- 0.1 vs 0.9 +/- 0.1 hours, P less than .0001). Group 1 children were significantly more likely to vomit AC than were group 2 children (18 of 32 vs six of 38, P less than .001). Patients receiving SOI who were subsequently discharged spent significantly more time in the ED than those receiving only AC (4.1 +/- 0.2 vs 3.4 +/- 0.2 hours, P less than .05). CONCLUSIONS: Ipecac delays the administration of AC, hinders its retention, and prolongs ED time in pediatric ingestion patients. These data support the recommendation that AC alone should be the gastrointestinal decontamination method of choice for the mild-to-moderate pediatric ingestion patient presenting to an ED.

Charcoal↗

Hydrated sodium calcium aluminosilicate (HSCAS), acidic HSCAS, and activated charcoal reduce urinary excretion of aflatoxin M1 in turkey poults. Lack of effect by activated charcoal on aflatoxicosis.

In one experiment, the effect of inorganic sorbents on the metabolic fate of aflatoxin B1 (AFB1) was studied in turkey poults. At 5 weeks of age, female poults were surgically colostomized and 9 days later orally dosed with 0.75 mg AFB1/kg BW. Hydrated sodium calcium aluminosilicate (HSCAS), acidic HSCAS, and activated charcoal (AC) were tested, by concomitant administration with AFB1. Urine was collected up to 48 h post-dosing and analyzed for aflatoxin M1 (AFM1) which was the major metabolite found in all treatment groups. Hydrated sodium calcium aluminosilicate, previously proven beneficial in alleviating aflatoxicosis in farm animals, reduced urinary AFM1 output when orally dosed simultaneous with AFB1. Also, acidic HSCAS and AC significantly decreased AFM1 excretion when administered concomitantly with AFB1. A second experiment was conducted to evaluate the ability of two types of AC to modify aflatoxicosis when added to aflatoxin (AF)-contaminated (from culture material) diets of turkey poults. Although AC was able to decrease AFM1 excretion in the first experiment, no protective effects from AF toxicity were observed in the feeding study.

Aflatoxin M1↗

Oral activated charcoal in the treatment of intoxications. Role of single and repeated doses.

Activated charcoal has an ability to adsorb a wide variety of substances. This property can be applied to prevent the gastrointestinal absorption of various drugs and toxins and to increase their elimination, even after systemic absorption. Single doses of oral activated charcoal effectively prevent the gastrointestinal absorption of most drugs and toxins present in the stomach at the time of charcoal administration. Known exceptions are alcohols, cyanide, and metals such as iron and lithium. In general, activated charcoal is more effective than gastric emptying. However, if the amount of drug or poison ingested is very large or if its affinity to charcoal is poor, the adsorption capacity of activated charcoal can be saturated. In such cases properly performed gastric emptying is likely to be more effective than charcoal alone. Repeated dosing with oral activated charcoal enhances the elimination of many toxicologically significant agents, e.g. aspirin, carbamazepine, dapsone, dextropropoxyphene, cardiac glycosides, meprobamate, phenobarbitone, phenytoin and theophylline. It also accelerates the elimination of many industrial and environmental intoxicants. In acute intoxications 50 to 100g activated charcoal should be administered to adult patients (to children, about 1 g/kg) as soon as possible. The exceptions are patients poisoned with caustic alkalis or acids which will immediately cause local tissue damages. To avoid delays in charcoal administration, activated charcoal should be a part of first-aid kits both at home and at work. The 'blind' administration of charcoal neither prevents later gastric emptying nor does it cause serious adverse effects provided that pulmonary aspiration in obtunded patients is prevented. In severe acute poisonings oral activated charcoal should be administered repeatedly, e.g. 20 to 50g at intervals of 4 to 6 hours, until recovery or until plasma drug concentrations have fallen to non-toxic levels. In addition to increasing the elimination of many drugs and toxins even after their systemic absorption, repeated doses of charcoal also reduce the risk of desorbing from the charcoal-toxin complex as the complex passes through the gastrointestinal tract. Charcoal will not increase the elimination of all substances taken. However, as the drug history in acute intoxications is often unreliable, repeated doses of oral activated charcoal in severe intoxications seem to be justified unless the toxicological laboratory has identified the causative agent as not being prone to adsorption by charcoal. The role of repeated doses of oral activated charcoal in chronic intoxication has not been clearly defined.(ABSTRACT TRUNCATED AT 400 WORDS)

Antidotes↗

Effect of ethanol and pH on the adsorption of acetaminophen (paracetamol) to high surface activated charcoal, in vitro studies.

BACKGROUND: Paracetamol (acetaminophen) intoxication often in combination with ethanol, is seen commonly in overdose cases. Doses of several grams might be close to the maximum adsorption capacity of the standard treatment dose (50g) of activated charcoal. The aim of this study was to determine the maximum adsorption capacity for paracetamol for two types of high surface-activated charcoal [Carbomix and Norit Ready-To-Use (not yet registered trademark in Denmark) both from Norit Cosmara, Amersfoort, The Netherlands] in simulated in vivo environments: At pH 1.2 (gastric environment), at pH 7.2 (intestinal environment), and with and without 10% ethanol. METHODS: Activated charcoal, at both gastric or intestinal pHs, and paracetamol were mixed, resulting in activated charcoal-paracetamol ratios from 10:] to 1:1. In trials with ethanol, some of the gastric or intestinal fluid was replaced with an equivalent volume of ethanol, resulting in an ethanol concentration of 10% v/v. After incubation, the concentration of unabsorbed paracetamol was analyzed by high-performance liquid chromatography. The maximum adsorption capacity of paracetamol to activated charcoal was calculated as mg paracetamol adsorbed/g activated charcoal, using Langmuir's isotherm. RESULTS: Carbomix [95% confidence limits are shown in square brackets]: 623.7 [612.8;634.5] mg paracetamol adsorbed/g activated charcoal (pH 1.2), 626.2 [611.6;640.9] mg paracetamol adsorbed/g activated charcoal (pH 7.2); Norit Ready-To-Use: 693.6 [676.8;710.5] mg paracetamol adsorbed/g activated charcoal (pH 1.2), 722.6 [687.4;757.9] mg paracetamol adsorbed/g activated charcoal (pH 7.2). For experiments with ethanol (10% v/v) the results with Carbomix were 465.7 [449.2;482.2] mg paracetamol adsorbed/g activated charcoal (pH 1.2), 498.6 [481.8;515.6] mg paracetamol adsorbed/g activated charcoal (pH 7.2); with Norit Ready-To-Use: 617.2 [606.6;627.7] mg paracetamol adsorbed/g activated charcoal (pH 1.2), 640.6 [624.9;656.4] mg paracetamol adsorbed/g activated charcoal (pH 7.2). CONCLUSION: Under conditions simulating immediate treatment with charcoal, a standard dose of 50 g of either of the two tested activated charcoals adsorbed a sufficient amount of paracetamol to be beneficial in the treatment of the majority of overdoses of this drug. For both types of activated charcoal, with or without ethanol, there was no significant difference in the adsorption of paracetamol at pH 1.2 and 7.2. Norit Ready-To-Use had a larger maximum adsorption capacity than Carbomix, and was not as sensitive as Carbomix to environmental changes (pH and ethanol). The presence of 10% ethanol lowered the adsorption capacity of the two tested activated charcoal preparations by an amount that might be clinically relevant in cases of intoxications by high-gram doses.

Acetaminophen↗

The adsorption of salicylates by a milk chocolate-charcoal mixture.

STUDY OBJECTIVE: To evaluate the adsorptive capacity of a milk chocolate-charcoal mixture to aspirin, compared with superactivated charcoal and conventional activated charcoal. DESIGN: A prospective, randomized, crossover study. SETTING: The Massachusetts Poison Control Center office in The Children's Hospital, Boston. TYPE OF PARTICIPANTS: Six healthy adult volunteers with no known allergies to aspirin or chocolate, bleeding disorders, or peptic ulcer disease. INTERVENTIONS: Each participant ingested 975 mg of crushed aspirin on separate days, followed by either water; 10 g milk chocolate-charcoal mixture; 10 g SuperChar Liquid; or 10 g Actidose Aqua activated charcoal. Total serum salicylate concentrations were determined by high-performance liquid chromatography at zero, one, two, four, eight, and 24 hours after ingestion. MEASUREMENTS AND MAIN RESULTS: Neuman-Keuls analysis was used to measure time-to-peak concentration, which was reduced by SuperChar Liquid, 67%; milk chocolate-charcoal mixture, 106%; and activated charcoal, 56%. Aspirin absorption was calculated using Neuman-Keuls analysis to measure area under the concentration-time curve. Total aspirin absorption was reduced by SuperChar, 67%; milk chocolate-charcoal mixture, 50%; and activated charcoal, 2%. There was no difference in serum salicylate concentrations between SuperChar and milk chocolate-charcoal mixture at all time intervals. Also, all serum salicylate concentrations with milk chocolate-charcoal mixture were consistently lower than with activated charcoal. CONCLUSION: Although the formulation of milk chocolate with activated charcoal reduces its adsorptive capacity compared with superactivated charcoal, it is still able to bind aspirin effectively and is superior to conventional activated charcoal. Further research may improve the binding and palatability of milk chocolate-charcoal mixture, especially for home use.

Adsorption↗